Disposition of 5-Aminosalicylic Acid by 5-Aminosalicylic Acid-Delivering Compounds

Rijk, M. C. M.; Schaik, A. Van; Tongeren, J. H. M. Van

doi:10.3109/00365528809101550

Cited by 40 publications

(24 citation statements)

References 25 publications

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“…Thus, only a small percentage of the oral dose is transported into the colon via the fecal stream and then is available to the colon mucosa. 11 In the light of these facts, in the present study, a five-or tenfold small dose (1 mg, 3 times weekly) of the oral dose (3 mg, daily) in our previous study 10 was selected for intrarectal administration of 5-ASA. Then, even this relatively small dose of 5-ASA administered intrarectally induced a protective effect against colon carcinogenesis, suggesting that a higher concentration of the active form of 5-ASA is available directly on the colon mucosa, as compared with the oral dose of 5-ASA.…”

Section: Discussionmentioning

confidence: 99%

Prevention by Intrarectal 5-Aminosalicylic Acid of N -Methylnitrosourea-Induced Colon Cancer in F344 Rats

Narisawa

Fukaura

2003

Diseases of the Colon &Amp; Rectum

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Section: Discussionmentioning

confidence: 99%

Prevention by Intrarectal 5-Aminosalicylic Acid of N -Methylnitrosourea-Induced Colon Cancer in F344 Rats

Narisawa

Fukaura

2003

Diseases of the Colon &Amp; Rectum

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“…Measurements of faecal contents may be difficult to interpret, however, because 5-ASA might be degraded by colonic bacteria to ac-5-ASA35 and to unknown products. 4 It has been shown that 5-ASA is the active anti-inflammatory moiety in chronic inflammatory bowel disease, whereas the acetylated metabolite seems inactive.3637 The uptake of 5-ASA in colonic cell preparations occurs rapidly and is equivalent to the production of ac-5-ASA by the cells, whereas the uptake of acetylated 5-ASA is slower.3 38 Not all 5-ASA penetrating the intestinal mucosa is acetylated, however, because our data confirm that a small portion also enters the systemic blood without prior acetylation.…”

Section: Intraluminal Phmentioning

confidence: 99%

Oroileal transit of slow release 5-aminosalicylic acid.

Goebell

Klotz

Nehlsen

et al. 1993

Gut

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The predominant active anti-inflammatory moiety in chronic inflammatory bowel disease is 5-aminosalicylic acid (5-ASA). As unprotected 5-ASA is rapidly absorbed in the upper gastrointestinal tract several slow release preparations have been developed to permit passage of 5-ASA to the lower small bowel and to the colon. To investigate luminal kinetics and extent ofthe release of 5-ASA intraluminal concentrations and loads of this compound together with that ofits main metabolite acetyl-5-aminosalicylic acid (ac-5-ASA) were studied, over 15 hours after giving the slow release preparation Salofalk at a dose of 500 mg orally together with a test meal. Plasma concentrations and urinary excretion were also measured. Six healthy volunteers swallowed an 11 lumen oroileal tube, which allowed marker perfusion, aspiration of luminal content from the duodenum, mid-jejunum, and ileum, and recording of intestinal motility. Emptying of 5-ASA into the duodenum started after emptying ofthe meal, together with the first phase III of interdigestive motility. Mean luminal concentrations of 5-ASA and ac-5-ASA increased continuously from duodenum (both: 15 to 30 [ig/ml) to ileum (60 to 110 tg/ml and 80 to 150 tg/ml respectively) over three hours and decreased over the next three hours. During 10 hours after eating, 30% of the total dose passed the ileum in solution and another 10% were excreted in urine. Thus about 60% reached the colon unreleased from tablets and another 30% were in solution. The ratio of 5-ASA and ac-5-ASA in solution was about 1:1 in the duodenum and 1:1-5 to 1:2 in the more distal small intestine. The data suggest that the large quantities of intraluminal ac-5-ASA are generated in the intestinal mucosa and reach the lumen by back diffusion. The results show that most of the 5-ASA from this slow release preparation is delivered into the colon, which explains its effectiveness in ulcerative colitis. The considerable luminal concentrations already present in the distal ileum might justify therapeutic trials in Crohn's disease.

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“…23,[35][36][37] As mentioned earlier, Ashford et al 23 reported the possible failure of mesalazine tablets coated with ES for colon-targeted delivery. A similar view was also expressed by Rijk et al 38 who studied few brands of commercially available pH-dependent mesalazine tablets in humans. It was also reported recently that the systems coated with pH-dependent polymer (ES) lacked site specificity for drug release in the colon and may either lead to a premature release of drug in the small intestine or no drug release in the colon.…”

Section: Optimization Of the Coating Layermentioning

confidence: 59%

Design and Optimization of Colon-Targeted System of Theophylline for Chronotherapy of Nocturnal Asthma

Patel

Amin

2011

Journal of Pharmaceutical Sciences

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Disposition of 5-Aminosalicylic Acid by 5-Aminosalicylic Acid-Delivering Compounds

Cited by 40 publications

References 25 publications

Prevention by Intrarectal 5-Aminosalicylic Acid of N -Methylnitrosourea-Induced Colon Cancer in F344 Rats

Prevention by Intrarectal 5-Aminosalicylic Acid of N -Methylnitrosourea-Induced Colon Cancer in F344 Rats

Oroileal transit of slow release 5-aminosalicylic acid.

Design and Optimization of Colon-Targeted System of Theophylline for Chronotherapy of Nocturnal Asthma

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